BGT226 (NVP-BGT226) - CAS 1245537-68-1
Catalog number:
1245537-68-1
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C28H25F3N6O2.C4H4O4
Molecular Weight:
650.6
COA:
Inquire
Targets:
PI3K
Description:
BGT226 (NVP-BGT226) is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.
Publictions citing BOC Sciences Products
  • >> More
Purity:
>98%
Synonyms:
N/A
MSDS:
Inquire
1.The novel dual PI3K/mTOR inhibitor NVP-BGT226 displays cytotoxic activity in both normoxic and hypoxic hepatocarcinoma cells.
Simioni C1,2, Cani A1,2, Martelli AM3, Zauli G4, Alameen AA1,5, Ultimo S1, Tabellini G6, McCubrey JA7, Capitani S1,2, Neri LM1. Oncotarget. 2015 Jul 10;6(19):17147-60.
Hepatocellular carcinoma (HCC) is one of the most common lethal human malignancies worldwide and its advanced status is frequently resistant to conventional chemotherapeutic agents and radiation. We evaluated the cytotoxic effect of the orally bioavailable dual PI3K/mTOR inhibitor, NVP-BGT226, on a panel of HCC cell lines, since hyperactivated PI3K/Akt/mTOR signaling pathway could represent a biomolecular target for Small Inhibitor Molecules in this neoplasia. We analyzed the drug activity in both normoxia and hypoxia conditions, the latter playing often a relevant role in the induction of chemoresistance and angiogenesis.In normoxia NVP-BGT226 caused cell cycle arrest in the G0/G1 phase of the cell cycle, induced apoptosis and autophagy at low concentrations. Interestingly the drug inactivated p-Akt and p-S6 at < 10 nM concentration.In hypoxia NVP-BGT226 maintained its cytotoxic efficacy at the same concentration as documented by MTT assays and Western blot analysis.
2.Synergistic anti-tumor effects of a novel phosphatidyl inositol-3 kinase/mammalian target of rapamycin dual inhibitor BGT226 and gefitinib in non-small cell lung cancer cell lines.
Katanasaka Y1, Kodera Y2, Yunokawa M2, Kitamura Y2, Tamura T3, Koizumi F4. Cancer Lett. 2014 Jun 1;347(2):196-203. doi: 10.1016/j.canlet.2014.02.025. Epub 2014 Mar 7.
Epidermal growth factor receptor (EGFR) and PI3K/mTOR pathway are drug targets for non-small cell lung cancer (NSCLC). Herein, we investigated anti-tumor effects of the combination of BGT226, a novel PI3K/mTOR dual inhibitor, and gefitinib on NSCLC cell lines which are high sensitive to gefitinib. The combination of BGT226 and gefitinib exhibited supra-additive growth inhibitory effects in PC-9 and HCC827 cells. Apoptotic induction and the inhibition of PI3K/mTOR signaling were enhanced by the combination. Significant tumor growth suppression was observed in xenograft model by the combination. These results suggest that the combination is effective in EGFR inhibitor-sensitive NSCLC therapy.
3.Cell cycle-dependent activity of the novel dual PI3K-MTORC1/2 inhibitor NVP-BGT226 in acute leukemia.
Kampa-Schittenhelm KM1, Heinrich MC, Akmut F, Rasp KH, Illing B, Döhner H, Döhner K, Schittenhelm MM. Mol Cancer. 2013 May 24;12:46. doi: 10.1186/1476-4598-12-46.
BACKGROUND: Dysregulation of the PI3Kinase/AKT pathway is involved in the pathogenesis of many human malignancies. In acute leukemia, the AKT pathway is frequently activated, however mutations in the PI3K/AKT pathway are uncommon. In some cases, constitutive AKT activation can be linked to gain-of-function tyrosine kinase (TK) mutations upstream of the PI3K/AKT pathway. Inhibitors of the PI3K/AKT pathway are attractive candidates for cancer drug development, but so far clinical efficacy of PI3K inhibitors against various neoplasms has been moderate. Furthermore, specific MTORC1 inhibitors, acting downstream of AKT, have the disadvantage of activating AKT via feed-back mechanisms. We now evaluated the antitumor efficacy of NVP-BGT226, a novel dual pan-PI3K and MTORC1/2 inhibitor, in acute leukemia.
4.NVP-BEZ235 and NVP-BGT226, dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitors, enhance tumor and endothelial cell radiosensitivity.
Fokas E1, Yoshimura M, Prevo R, Higgins G, Hackl W, Maira SM, Bernhard EJ, McKenna WG, Muschel RJ. Radiat Oncol. 2012 Mar 27;7:48. doi: 10.1186/1748-717X-7-48.
BACKGROUND: The phosphatidylinositol 3-kinase (PI3K)/Akt pathway is activated in tumor cells and promotes tumor cell survival after radiation-induced DNA damage. Because the pathway may not be completely inhibited after blockade of PI3K itself, due to feedback through mammalian target of rapamycin (mTOR), more effective inhibition might be expected by targeting both PI3K and mTOR inhibition.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related PI3K Products


CAS 648450-29-7 AS-605240

AS-605240
(CAS: 648450-29-7)

AS605240 is a selective PI3Kgamma inhibitor, has been proved effective on several inflammatory diseases. Orally administration of AS605240 significantly prevent...

CAS 1172118-03-4 PI3Ky inhibitor 1

PI3Ky inhibitor 1
(CAS: 1172118-03-4)

PI3Ky inhibitor 1 is a potent PI3Ky inhibitor.

CAS 944396-07-0 BKM120

BKM120
(CAS: 944396-07-0)

BKM120, also called as buparlisib or NVP-BKM120, activity in a range of preclinical cancermodels, specifically inhbits class I PI3K isoforms, which blocks p110α...

CAS 1372540-25-4 GSK2636771

GSK2636771
(CAS: 1372540-25-4)

GSK2636771 is an orally bioavailable, substituted benzimidazole inhibitor of the class I phosphoinositide 3-kinase (PI3K) beta isoform with potential antineopla...

CAS 19870-46-3 1,3-Dicaffeoylquinic acid

1,3-Dicaffeoylquinic acid
(CAS: 19870-46-3)

1,3-Dicaffeoylquinic acid, a caffeoylquinic acid derivative found in artichoke, acts as an anti-hyperlipidemic agent and activates PI3K/Akt.

PI3Kα inhibitor 1
(CAS: 1235449-52-1)

PI3Kα inhibitor 1 is an inhibitor of PI3Kα as well as HDAC and probably have antineoplastic activity. IC50: <0.1 μM.

IPI-549
(CAS: 1693758-51-8)

IPI-549, a dihydroisoquinolin derivative, has been found to be a phosphatidylinositol 3 kinase gamma inhibitor, could exhibit antineoplastic activity in solid t...

copanlisib hydrochloride
(CAS: 1402152-13-9)

Copanlisib hydrochloride is a potent inhibitor of Class I phosphoinositide 3-kinase which showed a therapeutic effect on non-Hodgkin lymphoma. It was approved t...

CAS 957054-33-0 GDC-0941 dimethanesulfonate

GDC-0941 dimethanesulfonate
(CAS: 957054-33-0)

GDC-0941 dimethanesulfonate is a potent inhibitor of PI3Kα/δ with modest selectivity against p110β and p110γ. It is a novel selective class I phosphatidylinosit...

CAS 1312445-63-8 NVP-BKM120 Hydrochloride

NVP-BKM120 Hydrochloride
(CAS: 1312445-63-8)

NVP-BKM120 Hcl(BKM120) is a selective PI3K inhibitor of p110&alpha;/&beta;/&delta;/&gamma; with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively.

CAS 1173900-33-8 AZD6482

AZD6482
(CAS: 1173900-33-8)

AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ. Phase 1.

CAS 371935-74-9 PI-103

PI-103
(CAS: 371935-74-9)

PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110α...

CAS 1245537-68-1 BGT226 (NVP-BGT226)

BGT226 (NVP-BGT226)
(CAS: 1245537-68-1)

BGT226 (NVP-BGT226) is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.

CAS 900185-02-6 PIK-294

PIK-294
(CAS: 900185-02-6)

PIK-294 is a potent PI3K inhibitor.

CAS 1166227-08-2 A66

A66
(CAS: 1166227-08-2)

Inhibition of p110α alone by A66 treatment is sufficient to block insulin signalling to Akt/PKB in certain cell lines that harbor H1047R mutations in PIK3CA and...

MLN1117
(CAS: 1268454-23-4)

MLN1117, also known as INK1117, is a PI3Kα inhibitor which could lead to the apoptosis and growth retardation of tumor cells expressed by PI3Kα. IC50: 15 nM.

CAS 1676893-24-5 NSC781406

NSC781406
(CAS: 1676893-24-5)

NSC781406 demonstrates potent PI3K inhibition (PI3Kα IC50=2.0 nM) and is a highly potent mTOR inhibitor, with reasonable liver microsome stability.

CAS 1201438-56-3 Duvelisib

Duvelisib
(CAS: 1201438-56-3)

Duvelisib, also known as IPI-145 and INK-1197, is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms o...

CAS 1332075-63-4 PI3k(delta) inhibitor 1

PI3k(delta) inhibitor 1
(CAS: 1332075-63-4)

PI3kδ inhibitor 1 is a potent and selective inhibitor of isoform of PI3Kδ; useful for treating disorders mediated by lipid kinases such as inflammation, immunol...

CAS 1349796-36-6 XL-765, SAR245409,

XL-765, SAR245409,
(CAS: 1349796-36-6)

Chemical Structure

CAS 1245537-68-1 BGT226 (NVP-BGT226)

Quick Inquiry

Verification code

Featured Items